Leucovorin

Administration

  • Type: Antidote; Chemotherapy Modulating Agent; Rescue Agent (Chemotherapy)
  • Dosage Forms: 5,10,15,25
  • Routes of Administration: IV, IM
  • Common Trade Names: Lederle Leucovorin

Adult Dosing

  • Fluorouracil adjuvant treatment, adv. colorectal CA
    • high dose: 200mg/m^2 IV QD x5 days
    • low dose: 20mg/m^2 IV QD x5 days
  • Leucovorin rescue, high-dose methotrexate
    • normal methotrexate elimination: 15mg PO/IM/IV q6h x10 doses
    • delayed late methotrexate elimination: 15mg PO/IM/IV q6h; Max: 25mg/dose PO, May give higher doses IM/IV
  • Delayed early methotrexate elimination and/or acute renal injury: 150mg IV q3h until methotrexate level <1 micromolar, then 15mg IV q3h
  • Leucovorin rescue, methotrexate overdose: 10mg/m^2 PO/IM/IV q6h
  • Folate antagonist overdose
    • pemetrexed: 50mg/m^2 IV q6h x8 days; Start: 100mg/m^2 IV x1
    • pyrimethamine, trimethoprim: 5-15mg PO/IM/IV QD until hematopoiesis restored
  • Megaloblastic anemia, folate-deficient: <1mg IM/IV QD
    • Max: 1mg/day

Pediatric Dosing

  • Leucovorin rescue, high-dose methotrexate
    • normal methotrexate elimination: 10mg/m^2 PO/IM/IV q6h x10 doses; Start: 24h after methotrexate start; Max: 25mg/dose PO
    • delayed late methotrexate elimination: 10mg/m^2 PO/IM/IV q6h; Max: 25mg/dose PO
    • delayed early methotrexate elimination and/or acute renal injury: 100mg/m^2 IV q3h until methotrexate level <1 micromolar, then 10mg/m^2 IV q3
  • Leucovorin rescue, methotrexate overdose: 10mg/m^2 PO/IM/IV q6h
  • Folate antagonist overdose: 5-15mg PO/IM/IV QD until hematopoiesis restored
  • Megaloblastic anemia, folate-deficient: <1mg IM/IV QD
    • Max: 1mg/day

Special Populations

  • Pregnancy Risk Factor: C
  • Breast Feeding: Leucovorin is a form of folic acid and is present in breast milk which may be beneficial to the newborn.

Renal Dosing

  • Not defined

Hepatic Dosing

  • Not defined

Contraindications

  • Allergy to class/drug
  • intrathecal administration
  • caution if pernicious anemia
  • caution if megaloblastic anemia, vitamin B12 deficient
  • caution if vitamin B-12 deficiency

Adverse Reactions

Serious

  • anaphylactoid reaction
  • seizures
  • syncope

Common

  • urticaria
  • nausea/vomiting (IV use)

Pharmacology

  • Half-life: 6hr
  • Metabolism: liver, GI, CYP450
  • Excretion: Urine

Mechanism of Action

Comments

See Also

References

<Epocrates, UpToDate>